EP2549276A3 - Couplage covalente et réversible de molecules fonctionelles - Google Patents

Couplage covalente et réversible de molecules fonctionelles Download PDF

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Publication number
EP2549276A3
EP2549276A3 EP12189317A EP12189317A EP2549276A3 EP 2549276 A3 EP2549276 A3 EP 2549276A3 EP 12189317 A EP12189317 A EP 12189317A EP 12189317 A EP12189317 A EP 12189317A EP 2549276 A3 EP2549276 A3 EP 2549276A3
Authority
EP
European Patent Office
Prior art keywords
formula
covalent linkage
functional molecules
reversible covalent
present
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP12189317A
Other languages
German (de)
English (en)
Other versions
EP2549276B1 (fr
EP2549276A2 (fr
Inventor
Mark Smith
Stephen Caddick
James Baker
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
UCL Business Ltd
Original Assignee
UCL Business Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0913967A external-priority patent/GB0913967D0/en
Priority claimed from GB0913965A external-priority patent/GB0913965D0/en
Priority claimed from GB0914321A external-priority patent/GB0914321D0/en
Application filed by UCL Business Ltd filed Critical UCL Business Ltd
Priority to DK15150363.8T priority Critical patent/DK2889624T3/en
Priority to EP15150363.8A priority patent/EP2889624B1/fr
Publication of EP2549276A2 publication Critical patent/EP2549276A2/fr
Publication of EP2549276A3 publication Critical patent/EP2549276A3/fr
Application granted granted Critical
Publication of EP2549276B1 publication Critical patent/EP2549276B1/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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    • AHUMAN NECESSITIES
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    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545Heterocyclic compounds
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    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
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    • A61K47/56Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/36Oxygen or sulfur atoms
    • C07D207/402,5-Pyrrolidine-diones
    • C07D207/4162,5-Pyrrolidine-diones with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/456Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/655Somatostatins
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
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    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
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  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
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  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
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  • Oncology (AREA)
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  • General Physics & Mathematics (AREA)
EP12189317.6A 2009-08-10 2010-08-09 Couplage covalente et réversible de molecules fonctionelles Active EP2549276B1 (fr)

Priority Applications (2)

Application Number Priority Date Filing Date Title
DK15150363.8T DK2889624T3 (en) 2009-08-10 2010-08-09 Reversible covalent bonding of functional molecules
EP15150363.8A EP2889624B1 (fr) 2009-08-10 2010-08-09 Liaison covalente réversible de molécules fonctionnelles

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB0913967A GB0913967D0 (en) 2009-08-10 2009-08-10 Functionalisation of solid substrates
GB0913965A GB0913965D0 (en) 2009-08-10 2009-08-10 Reversible covalent linkage of functional moieties
GB0914321A GB0914321D0 (en) 2009-08-14 2009-08-14 Thiol protecting group
EP10742867A EP2464972A1 (fr) 2009-08-10 2010-08-09 Liaison colavente réversible de molécules fonctionnelles

Related Parent Applications (2)

Application Number Title Priority Date Filing Date
EP10742867A Division EP2464972A1 (fr) 2009-08-10 2010-08-09 Liaison colavente réversible de molécules fonctionnelles
EP10742867.4 Division 2010-08-09

Related Child Applications (2)

Application Number Title Priority Date Filing Date
EP15150363.8A Division-Into EP2889624B1 (fr) 2009-08-10 2010-08-09 Liaison covalente réversible de molécules fonctionnelles
EP15150363.8A Division EP2889624B1 (fr) 2009-08-10 2010-08-09 Liaison covalente réversible de molécules fonctionnelles

Publications (3)

Publication Number Publication Date
EP2549276A2 EP2549276A2 (fr) 2013-01-23
EP2549276A3 true EP2549276A3 (fr) 2013-03-20
EP2549276B1 EP2549276B1 (fr) 2015-02-25

Family

ID=42668730

Family Applications (5)

Application Number Title Priority Date Filing Date
EP10744980A Withdrawn EP2464974A1 (fr) 2009-08-10 2010-08-09 Fonctionnalisation de substrats solides
EP10747930.5A Not-in-force EP2464654B1 (fr) 2009-08-10 2010-08-09 Groupement protecteur thiol
EP15150363.8A Active EP2889624B1 (fr) 2009-08-10 2010-08-09 Liaison covalente réversible de molécules fonctionnelles
EP10742867A Withdrawn EP2464972A1 (fr) 2009-08-10 2010-08-09 Liaison colavente réversible de molécules fonctionnelles
EP12189317.6A Active EP2549276B1 (fr) 2009-08-10 2010-08-09 Couplage covalente et réversible de molecules fonctionelles

Family Applications Before (4)

Application Number Title Priority Date Filing Date
EP10744980A Withdrawn EP2464974A1 (fr) 2009-08-10 2010-08-09 Fonctionnalisation de substrats solides
EP10747930.5A Not-in-force EP2464654B1 (fr) 2009-08-10 2010-08-09 Groupement protecteur thiol
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AU2010283632A1 (en) 2012-03-08
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